RESUMO
Little is known about the relationship between traffic congestion and antimony (Sb) distribution in street dust, which is essential for Sb control and emission reduction in urban areas. Sb concentrations and mass load of the street dust collected in 19 cities of China were determined before investigating the mechanism of traffic influence on Sb distribution through diverse statistical means. The results showed that the Sb concentrations in each city were 1.10-4.76 times higher than the local background values. Sb concentrations in transportation areas were significantly higher than those in residential and industrial areas, and were significantly affected by road network density. The effect of congestion on Sb load of street dust was influenced by vehicle flowrate. Only when the vehicle flowrate was high, the traffic congestion would promote the increase of Sb load obviously. The improved accounting method showed that the Sb dissipation from brake wear in major Chinese cities were higher than that in Stockholm, Sweden, in 2005. The latent path analysis illustrated that a 1% increase in congestion index was correlated with a 0.886% increase in the Sb load. Compared with Switzerland, which has a typical industrialized Sb consumption pattern, China needs to recycle brake pads in addition to taking various measures to alleviate traffic congestion and reduce brake pad wear, despite the fact that the maximum health risk of Sb was far below the safety threshold. This study will provide valuable insights for urban traffic management and brake pad recycling.
Assuntos
Poeira , Metais Pesados , Antimônio/análise , Cidades , Poeira/análise , Monitoramento Ambiental , Humanos , Metais Pesados/análise , Meios de TransporteRESUMO
Two new dimeric 1,4-benzoquinone derivatives, peniquinone A (1) and peniquinone B (2), a new dibenzofuran penizofuran A (3), and a new pyrazinoquinazoline derivative quinadoline D (4), together with 13 known compounds (5-17), were isolated from a marine-derived fungus Penicillium sp. L129. Their structures, including absolute configurations, were elucidated by extensive spectroscopic data and electronic circular dichroism calculations. Compound 1 exhibited cytotoxicity against the MCF-7, U87 and PC3 cell lines with IC50 values of 12.39 µM, 9.01 µM and 14.59 µM, respectively, while compound 2 displayed relatively weak cytotoxicity activities against MCF-7, U87 and PC3 cell lines with IC50 values of 25.32 µM, 13.45 µM and 19.93 µM, respectively. Furthermore, compound 2 showed weak quorum sensing inhibitory activity against Chromobacterium violaceum CV026 with an MIC value of 20 µg/well.
Assuntos
Antineoplásicos/farmacologia , Organismos Aquáticos/química , Benzoquinonas/farmacologia , Penicillium/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Benzoquinonas/química , Benzoquinonas/isolamento & purificação , Linhagem Celular Tumoral , Chromobacterium/efeitos dos fármacos , Chromobacterium/fisiologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Percepção de Quorum/efeitos dos fármacosRESUMO
The natural chimeric gene is a novel gene fused by two or more independent genes. Its discovery extends the classical gene concept that one gene resides in one chromosomal locus. During tumorigenesis, many chimeric genes lead to tumor-related diseases; therefore, it is one molecular marker for cancer diagnosis. In this review, we summarize the research progress of chimeric genes in terms of their feature, structure, transcription, regulation and function. We pinpoint the difficulties and challenges in the current research work, and discuss the application of chimeric gene in the new gene design.
Assuntos
Transformação Celular Neoplásica/genética , Rearranjo Gênico , Neoplasias/genética , Proteínas de Fusão Oncogênica/genética , Animais , Transformação Celular Neoplásica/metabolismo , Regulação da Expressão Gênica , Engenharia Genética/métodos , Humanos , Neoplasias/metabolismo , Proteínas de Fusão Oncogênica/metabolismo , Translocação GenéticaRESUMO
With excessive Mn(â ¡) and Cu(â ¡) pollution in aquatic environments posing potential health risks to inhabitants, the emergence of carbon capture, utilization and storage (CCUS) technology has promoted the improvement of heavy metal remediation technologies. Using hydrothermal sediment as a crystal seed, rhamnolipid was used to mediate biomimetic mineralization to prepare hydrated magnesium carbonate (HMC) composites to enhance the Mn(â ¡)/Cu(â ¡) adsorption performance of alginate hydrogels. Hydrothermal sediment is beneficial for accelerating biomimetic mineralization, while rhamnolipid can induce a crystalline phase transformation from dypingite to nesquehonite. The addition of sediment significantly enhanced the compressive mechanical properties and thermal stability of the hydrogels. The adsorption performances of the nesquehonite and dypingite hydrogels were better for Mn(II) and Cu(II), respectively. An increase in the amount of sediment improved the adsorption of Cu(II) by the hydrogels appropriately, resulting in stronger selectivity for Cu(II). The adsorption of Mn(II) and Cu(II) on the hydrogel beads was thermodynamically spontaneous. The inhibitory effects of sodium dodecyl benzene sulfonate (SDBS), fulvic acid (FA) and alginate on Cu(II) adsorption were more obvious than those of bovine serum albumin (BSA). Both the complexation of functional groups on alginate and mineralization by HMC participated in the adsorption of Mn(II) and Cu(II).
RESUMO
The common use of peroxides in the remediation of malodorous black water may lead to the activation of heavy metals in sediment when eliminating black and odorous substances. The mechanisms of heavy metal interactions with dissolved organic matter (DOM) in response to in situ capping have not been elucidated, but this information could guide the optimization of capping materials. We developed a capping material consisting of hydrothermally carbonized sediment (HCS), hydrated magnesium carbonate (HMC) and sodium percarbonate (SPC) and used microcosm experiments to investigate the dynamics of Mn and Cu at the sediment-water interface in malodorous black water. The results showed that HCS, HMC and SPC contributed multiple functions of mechanical protection, chemical isolation and oxygen provision to the new caps. HMC promoted the conversion of Mn/Cu into carbonate minerals. The optimal mass proportions were 25 % HCS, 60 % HMC and 15 % SPC based on the mixture design. In situ capping altered the fate and transformation of metals in the sediment-overlying water profile in the short term through Mn immobilization and Cu activation. The complexation of Cu(II) ions was significantly stronger than that of Mn(II) ions. In situ capping had a significant effect on the order of complexation of different fluorescent DOM molecules with Mn(II)/Cu(II) ions: microbial byproducts and fulvic acid-like components were preferentially complexed with Cu(II) ions after capping, while phenolic and humic acid-like components preferentially interacted with Mn(II) ions. Humic-like components bound to Cu were affected the most by capping treatment, whereas protein-like components were relatively weakly affected. Our study provides valuable knowledge on the impact of in situ capping on DOM-metal complexes.
Assuntos
Matéria Orgânica Dissolvida , Metais Pesados , Metais Pesados/química , Substâncias Húmicas/análise , Íons , Espectrometria de Fluorescência/métodosRESUMO
Three new formyl phloroglucinol meroterpenoids, eumaidials A-C (1-3), were isolated from the leaves of Eucalyptus globulus subsp. maidenii, along with ten known analogues (4-13). Their chemical structures were determined by various spectral data and electronic circular dichroism calculations. Eumaidial A (1) is the first ß-caryophyllene-based formyl phloroglucinol meroterpenoids from the genus Eucalyptus. Compounds 1-4 and 10 exhibited ATP-citrate lyase inhibitory activities, and compounds 2 and 3 suppressed the hepatocyte lipogenesis.
Assuntos
Eucalyptus , Complexos Multienzimáticos , Oxo-Ácido-Liases , Estrutura Molecular , Eucalyptus/química , Floroglucinol/farmacologia , Floroglucinol/química , Folhas de Planta/química , Trifosfato de AdenosinaRESUMO
AIM: Fatty acid-binding protein 4 (FABP4) plays an important role in maintaining glucose and lipid homeostasis. The aim of this study was to find new inhibitors of FABP4 for the treatment of type 2 diabetes. METHODS: Human FABP4 protein was expressed, and its inhibitors were detected in 1,8-ANS displacement assay. The effect of the inhibitor on lipolysis activity was examined in mouse 3T3-L1 preadipocytes. The db/db mice were used to evaluate the anti-diabetic activity of the inhibitor. Molecular docking and site-directed mutagenesis studies were carried out to explore the binding mode between the inhibitor and FABP4. RESULTS: From 232 compounds tested, benzbromarone (BBR), an old uricosuric drug, was discovered to be the best inhibitor of FABP4 with an IC50 value of 14.8 µmol/L. Furthermore, BBR (25 µmol/L) significantly inhibited forskolin-stimulated lipolysis in 3T3-L1 cells. Oral administration of BBR (25 or 50 mg/kg, for 4 weeks) dose-dependently reduced the blood glucose level and improved glucose tolerance and insulin resistance in db/db mice. Molecular docking revealed that the residues Ser55, Asp76, and Arg126 of FABP4 formed important interactions with BBR, which was confirmed by site-directed mutagenesis studies. CONCLUSION: BBR is an inhibitor of FABP4 and a potential drug candidate for the treatment of type 2 diabetes and atherosclerosis.
Assuntos
Benzobromarona/farmacologia , Glicemia/efeitos dos fármacos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Proteínas de Ligação a Ácido Graxo/antagonistas & inibidores , Células 3T3-L1 , Animais , Benzobromarona/administração & dosagem , Relação Dose-Resposta a Droga , Teste de Tolerância a Glucose , Humanos , Concentração Inibidora 50 , Resistência à Insulina , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Simulação de Acoplamento Molecular , Mutagênese Sítio-Dirigida , Uricosúricos/administração & dosagem , Uricosúricos/farmacologiaRESUMO
Strains representing a novel ascomycetous yeast species, Candida sanyaensis, were isolated from soil samples collected on Hainan Island and Taiwan Island in China. Analysis of the D1/D2 domains of the large subunit (LUS) rRNA gene and internal transcribed spacer (ITS) regions of these strains showed that this species was related to Candida tropicalis and Candida sojae, their closest relatives. C. sanyaensis differed by three substitutions and one gap from C. tropicalis, and by four substitutions and one gap from C. sojae, in the D1/D2 domain sequences. However, the ITS sequences of C. sanyaensis were quite divergent from the latter two species, showing that it is a genetically separate species. The novel strains were also found to have very similar PCR-fingerprinting profiles which were quite distinct from those of C. tropicalis and C. sojae strains. The type strain of C. sanyaensis is HN-26(T) (= CICC 1979(T) = CBS 12637(T)).
Assuntos
Candida/classificação , Candida/isolamento & purificação , Microbiologia do Solo , Candida/citologia , Candida/genética , China , Análise por Conglomerados , DNA Fúngico/química , DNA Fúngico/genética , DNA Ribossômico/química , DNA Ribossômico/genética , DNA Espaçador Ribossômico/química , DNA Espaçador Ribossômico/genética , Genes de RNAr , Microscopia , Dados de Sequência Molecular , Técnicas de Tipagem Micológica , Filogenia , RNA Fúngico/genética , RNA Ribossômico/genética , Análise de Sequência de DNARESUMO
Two strains of a novel basidiomycetous yeast species were isolated from the gut of wood-boring larvae collected in the Baotianman Nature Reserve, the central China. Sequence analysis of the D1/D2 domains of the large subunit (LSU) rRNA gene and internal transcribed spacer (ITS) regions showed that these yeasts belong to the Bulleromyces clade and formed a cluster together with eleven undescribed Cryptococcus species. The novel species differed from its closest known species, Cryptococcus rajasthanensis, by 3.3 % divergence (15 substitutions and 6 gaps over 630 bases) in the D1/D2 domains, and by 13.4 % divergence (41 substitutions and 27 gaps over 508 bases) in the ITS regions. Physiologically, the fermentation of glucose, galactose, sucrose, trehalose, and raffinose in Durham tubes was observed for the strains of this new yeast. Based on the phenotypical and molecular characteristics presented, the two strains are proposed as a new species, Cryptococcus nanyangensis sp. nov., with the type strain KCY-1(T) (=CICC 1976(T) = CBS 12474(T)).
Assuntos
Cryptococcus/classificação , Cryptococcus/isolamento & purificação , Trato Gastrointestinal/microbiologia , Larva/microbiologia , Leveduras/isolamento & purificação , Animais , China , Cryptococcus/genética , Dados de Sequência Molecular , Filogenia , Populus/parasitologia , Quercus/parasitologia , Madeira/parasitologia , Leveduras/classificação , Leveduras/genéticaRESUMO
OBJECTIVE: To study the gene expression of Notch1 and Jagged1 in children with acute leukemia (AL) and their possible roles in the pathogenesis of AL. METHODS: Mononuclear cells from bone marrow or peripheral blood of 47 children with AL and 20 controls (normal children or children with nonmalignant hematologic disease) were collected from February 2009 to July 2011. A two-step method to semi-quantitative reverse transcription-polymerase chain reaction (RT-PCR) was used to detect the gene expression of Notch1 and Jagged1. Of the 47 children with AL, there were 26 cases of B-ALL, 6 cases of T-ALL and 15 cases of AML. RESULTS: The positive expression rate of Notch1 in the ALL and AML groups was higher than in the control group (P<0.05). The expression level of Notch1 in T-ALL children was higher than in B-ALL children (P<0.01). The positive expression rate of Jagged1 in the ALL and AML groups was not significantly different from the control group, however, the expression level of Jagged1 in the ALL and AML groups was higher than in the control group (P<0.05). CONCLUSIONS: There are significant differences in the gene expression of Notch1 between children with different types of ALL, and a higher expression of Notch1 relates to T-ALL. The activation of Notch1 signal is common in children with AL. The abnormal gene expression of Notch1 in children with AML shows the role of Notch1 in AML. The gene expression of Jagged1 in children with ALL or AML is abnormal, and this needs to be confirmed by further research.
Assuntos
Proteínas de Ligação ao Cálcio/genética , Regulação Neoplásica da Expressão Gênica , Peptídeos e Proteínas de Sinalização Intercelular/genética , Leucemia/metabolismo , Proteínas de Membrana/genética , Receptor Notch1/genética , Doença Aguda , Adolescente , Criança , Pré-Escolar , Feminino , Humanos , Lactente , Proteína Jagged-1 , Leucemia Mieloide Aguda/metabolismo , Leucemia-Linfoma de Células T do Adulto/metabolismo , Masculino , Receptor Notch1/metabolismo , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Proteínas Serrate-Jagged , Transdução de SinaisRESUMO
Spatiotemporal variability complicates source apportionment of metals in urban lakes, especially when rainfall drives urban non-point source pollution. As, Cd, Cr, Pb, Hg, Ag, Co, Cu, Fe, Mn, Ni, Sb, Sr and Zn concentrations in 648 water samples collected before and after rain in 6 urban lakes of Beijing, China were determined during 2013-2015. The response of metals concentrations after rain to the interaction between rainfall and antecedent dry days was significant. Metals concentrations were normalized pursuant to the interaction effect as the input of positive matrix factorization (PMF) to develop the interaction normalized-PMF (IN-PMF). Four primary pollution sources were diagnosed. Sediment release was considered to be the main source of Fe, Co and Ni independent of rainfall. Hg, As and some Cr associated with pesticides and fertilizers were likely to come from soil erosion and runoff from green space. It is probable that road runoff was the dominant source for heavy metals related to traffic emissions, including Pb, Cd, Cu, Sb, Mn and Zn. Cr, Sr and some Cu and Zn as key elements of rooftops can be regarded as from roof runoff. The IN-PMF lowered roof and road runoff contributions and raised the contribution of soil erosion from green space, with Pb, Sb, Cu, Zn, Cd and Mn increasing by 15.9%, 10.7%, 13.1%, 12.2%, 13.3% and 16.8%. The results shed more light on the stormwater runoff pollution mitigation on impervious surfaces and metals enrichment problems in infiltration soil on green space in the low impact development (LID) setting. The Bayesian network revealed the spatial variability of transport and fate of metal elements from land surfaces to urban lakes, supplementing the secondary pollution sources from different land use. This study will provide new insights for source apportionment of non-point source pollution under the background of sponge city construction.
Assuntos
Mercúrio , Metais Pesados , Poluição Difusa , Poluentes do Solo , Teorema de Bayes , Cádmio , China , Monitoramento Ambiental/métodos , Lagos , Chumbo , Metais Pesados/análise , Medição de Risco , Solo , Poluentes do Solo/análiseRESUMO
Glycosylated natural products are reliable platforms for the development of anticancer drugs, simply due to the important features added by sugar appendages to the shape and the stereoelectronic properties of natural scaffolds. Herein, we indentified D11, a novel diphyllin glycoside with acetylated D-quinovose sugar moiety, as a potent topoisomerase IIα (Topo IIα) inhibitior. This peculiar sugar moiety endows D11 an optimal conformation with a high binding affinity for Topo IIα via hydrogen bonding to the entrance of ATPase pocket, thereby helping achieve more potent Topo II inhibition activity compared to the aglycon diphyllin. Further biochemical insights manifested that D11 significantly inhibited Topo IIα ATPase-catalyzed ATP hydrolysis in an ATP-dependent, but a DNA-independent manner. All these underlie the consequent superiority of D11 in the in vitro proliferation inhibition, apoptosis induction and the in vivo remarkable antitumor potency in xenograft mouse model. Moreover, D11 treatment also displayed no obvious body weight loss and other apparent toxicities, indicative of the restricted side effects by the virtue of sugar attachment. Taken together, a defined glycosylated manipulation of diphyllin may be a promising alternative approach in the development of novel Topo II inhibitors.
Assuntos
Antineoplásicos/farmacologia , Proteínas de Ligação a DNA/antagonistas & inibidores , Dioxolanos/farmacologia , Glucosídeos/farmacologia , Lignanas/farmacologia , Adenosina Trifosfatases/metabolismo , Trifosfato de Adenosina/metabolismo , Animais , Antígenos de Neoplasias/química , Antígenos de Neoplasias/metabolismo , Antineoplásicos/química , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Benzodioxóis , Biocatálise/efeitos dos fármacos , Linhagem Celular Tumoral , DNA/metabolismo , DNA Topoisomerases Tipo I/metabolismo , DNA Topoisomerases Tipo II/química , DNA Topoisomerases Tipo II/metabolismo , Proteínas de Ligação a DNA/química , Proteínas de Ligação a DNA/metabolismo , Dioxolanos/química , Dioxolanos/toxicidade , Feminino , Glucosídeos/química , Glucosídeos/toxicidade , Glicosilação/efeitos dos fármacos , Humanos , Hidrólise/efeitos dos fármacos , Lignanas/química , Lignanas/toxicidade , Camundongos , Camundongos Endogâmicos BALB C , Inibidores da Topoisomerase II/química , Inibidores da Topoisomerase II/farmacologia , Inibidores da Topoisomerase II/toxicidade , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
BACKGROUND: Cisplatin (CDDP) is a drug used for treatment of many types of malignancy but pancreatic cancer is relatively resistant to it. This study aims to determine whether and how cyclin D1 (D1) and c-Myc influence the response of pancreatic cancer cells to CDDP. MATERIALS AND METHODS: Ela-mycPT mouse pancreatic cancer cells were transfected with D1 or c-myc cDNA and treated with CDDP alone or together with NPCD, an inhibitor of cyclin dependent ckinase (CDK) 4 and 6. Reverse transcription followed by polymerase chain reaction (RT-PCR) and western blot assays were used to determine the mRNA and protein levels of interested genes. Cell viability was determined using 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. RESULTS: Treatment of Ela-mycPT1 cells with CDDP caused an increase in c-myc expression but a slightly latent decrease in D1 expression, whereas D1 and c-Myc proteins repressed each other. D1 or c-Myc rendered Ela-mycPT1 cells resistant or sensitive, respectively, to CDDP. D1 induced the expression of several members of the NF-κB family, including RelA, RelB, Nfκb1 and Nfκb2. D1 also induced BIRC5 and several pro-survival members of the Bcl-2 gene family, including Bcl-2 , Mcl-1 and Bad while it decreased the level of the pro-apoptotic Noxa. Inhibition of CDK4 or CDK6 kinase activity by NPCD did not affect these effects of D1. In contrast, c-Myc in Ela-mycPT1 and Ela-mycPT4 cells has the opposite effects to D1 on the expression of most of these apoptosis regulating genes. CONCLUSION: Our results suggest that induction of c-Myc and inhibition of D1 may be mechanisms for CDDP to elicit cytotoxicity. On the other hand, D1 induces whereas c-Myc represses the expression of key NF-κB family members to induce and repress, respectively, the expression of BIRC5 and several Bcl-2 family members, in turn inhibiting or enhancing the response to CDDP.
RESUMO
Rosiglitazone has been reported to exert dual effects on liver steatosis, and it could exacerbate liver steatosis in obese animal models, which was suggested to be closely related to the elevated hepatic expression of FABP4. This study aimed to investigate whether combined treatment with FABP4 inhibitor I-9 could alleviate rosiglitazone-induced liver steatosis in obese diabetic db/db mice. Male C57BL/KsJ-db/db mice were orally treated with rosiglitazone, rosiglitazone combined with I-9 daily for 8 weeks. The liver steatosis was evaluated by triglyceride content and H&E staining. The expression of hepatic lipogenic genes or proteins in liver tissue or in FFA-treated hepatocytes and PMA-stimulated macrophages were determined by real-time quantitative polymerase chain reaction (RT-qPCR) or western blotting. Results showed that combined treatment with I-9 decreased rosiglitazone-induced increase in serum FABP4 level and expression of lipogenic genes in liver, especially FABP4, and ameliorated liver steatosis in db/db mice. Rosiglitazone-induced intracellular TG accumulation and increased expression of FABP4 in the cultured hepatocytes and macrophages were also suppressed by combined treatment. We concluded that combined treatment with FABP4 inhibitor I-9 could ameliorate rosiglitazone-exacerbated elevated serum FABP4 level and ectopic liver fat accumulation in obese diabetic db/db mice without affecting its anti-diabetic efficacy.
Assuntos
Proteínas de Ligação a Ácido Graxo/antagonistas & inibidores , Fígado Gorduroso/tratamento farmacológico , Rosiglitazona/farmacologia , Animais , Diabetes Mellitus Tipo 2/complicações , Combinação de Medicamentos , Proteínas de Ligação a Ácido Graxo/sangue , Proteínas de Ligação a Ácido Graxo/metabolismo , Fígado Gorduroso/etiologia , Fígado Gorduroso/patologia , Hepatócitos/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Modelos Animais , Obesidade/complicações , Cultura Primária de Células , Triglicerídeos/metabolismoRESUMO
In the process of lignin extraction by the organic solvent method, the amount of alkali and the content of 1,4-butanediol are important conditions that affect lignin yield. The effects of alkali and alcohol contents on lignin recovery, removal rate, and structure were studied. In this reaction system, the removal rate of lignin increased with the increase of alkali content but decreased with the increase of alcohol content. Fourier transform infrared (FT-IR) analysis showed that the phenol hydroxyl group and the ether bond in lignin had different trends in different alkali and 1,4-butanediol environments, and four different infrared parameters in lignin had an obvious linear relationship. Gel permeation chromatography (GPC) results showed that high alkali content and high 1,4-butanediol content could lead to the fragmentation of lignin. In addition, lignin extracted from alkali-quantity factor series was selected to prepare activated carbon, CaCl2 was selected as the activator, and its effects were studied. Results showed that in the process of extracting lignin, on the one hand, NaOH content affects the functional groups of activated carbon by affecting the aromatic structure of lignin; on the other hand, the NaOH content affects the graphitization degree and specific surface area of activated carbon by affecting the removal rate and the molecular weight of lignin.
RESUMO
Fatty acid-binding protein 4 (FABP4) and fatty acid-binding protein 5 (FABP5) are promising therapeutic targets for the treatment of various metabolic diseases. However, the weak potency, low selectivity over FABP3, or poor pharmacokinetic profiles of currently reported dual FABP4/5 inhibitors impeded further research. Here, we described the characterization of a series of dual FABP4/5 inhibitors with improved metabolic stabilities and physicochemical properties based on our previous studies. Among the compounds, D9 and E1 exhibited good inhibitory activities against FABP4/5 and favorable selectivity over FABP3 in vitro. In cell-based assays, D9 and E1 exerted a decrease of FABP4 secretion, a strong anti-lipolytic effect in mature adipocytes, and suppression of MCP-1 expression in THP-1 macrophages. Moreover, D9 and E1 possessed good metabolic stabilities in mouse hepatic microsomes and acceptable pharmacokinetics profiles in ICR mice. Further in vivo experiments showed that D9 and E1 could potently decrease serum FABP4 levels and ameliorate glucose metabolism disorders in obese diabetic db/db mice. These results demonstrated that D9 and E1 could serve as lead compounds for the development of novel anti-diabetic drugs.
Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Proteínas de Ligação a Ácido Graxo/uso terapêutico , Animais , Proteínas de Ligação a Ácido Graxo/farmacologia , Humanos , Camundongos , Estrutura MolecularRESUMO
OBJECTIVE: To understand the epidemic condition, distribution and biological characteristics of non-O1/non-O139 Vibrio cholerae from 2001 to 2009 in Haizhu District, to provide a scientific basis for the prevention and control of acute diarrhea. METHODS: Referring to the detecting method written in "Cholera control handbook" in the fifth edition, 764 specimens from outside environment (including the water in the Pearl River, drinking water, water for breeding fish, aquatic products and delicatessen foods), 189 specimens of healthy population and 3398 intestinal samples of patients with diarrhea, summing up to 4351 specimens for non-O1/non-O139 Vibrio cholerae test. RESULTS: 4,351 specimens were detected of 101 strains of non O1/non O139 Vibrio cholerae, the total detection rate was 2.32%; 66 strains were identified by serotyping and grouped into 26 different serotypes, the typing rate was 65.3%. The strains VBO9, VBO38 and VBO76 were the dominant bacteria.Nine strains of the same type of non-O1/non-O139 Vibrio cholerae were found from external environments also from patients with diarrhea, suggesting that there might be a correlation between the two. CONCLUSION: Non-O1/non-O139 Vibrio cholerae have diversified serotypes, causing certain infection rate among the population in this region. These bacteria exist extensively in external environment and they are the potential hazard to the citizens.
Assuntos
Cólera/epidemiologia , Cólera/microbiologia , Vibrio cholerae , China/epidemiologia , Humanos , Sorotipagem , Vibrio cholerae/classificação , Vibrio cholerae/isolamento & purificaçãoRESUMO
Lead (Pb) is an important pollutant and it is of significance to explore the Pb distribution, influencing factors and health risk. Pb concentration and mass load per unit area in 385 street dust samples collected from 19 cities in China were determined during 2011-2013. The results show that the Pb concentration are 68.8, 105.4, 41.7, 49.7, 75.6, 81.7, 131.9, 67.5, 109.3, 164.1, 74.8, 66.4, 99.8, 58.4, 114.0, 59.6, 103.7, 55.4 and 80.4 for Beijing, Chengdu, Daqing, Harbin, Jilin, Jinan, Kunming, Lanzhou, Luoyang, Panzhihua, Qingdao, Yinchuan, Guangzhou, Tangshan, Xi'an, Guangyuan, Nanjing, Taiyuan and Tianjin, respectively. The Pb pollution level of urban street dust varies among cities in the range of 1.72-5.56 times higher than soil background values. The allometric function can fit the change in Pb concentration with particle size well. The medium-sized (38-120 µm) particles contributed 60.2%-80.4% to the Pb load and should be highlighted when selecting street dust management techniques. Influenced by the distribution of Pb ore, the Pb concentration of urban street dust in China shows obvious regional differences, with value in the south 112% higher than that in the north. Among all kinds of mining types, metal-related mining activities discharge a large amount of Pb dust in the process of crushing and smelting, thus contributing most to the Pb load. The Pb load was also affected by transportation. The relationship between Pb load and gross domestic product (GDP) was described with the environmental Kuznets curve (EKC) model, which indicated that the Pb emissions of most cities were still increasing. Finally, the human health risk assessment model with adjusted parameters showed that the Pb risk of all cities was below the threshold. Despite all this, given the EKC law of Pb emission, long-term follow-up assessments are needed.
Assuntos
Poeira/análise , Metais Pesados/análise , Pequim , China , Cidades , Monitoramento Ambiental , Produto Interno Bruto , Humanos , Medição de RiscoRESUMO
A new γ-pyrone derivative, acrepyrone A (1), and three known sorbicillinoids, trichodimerol (2), dihydrotrichodimerol (3) and tetrahydrotrichodimerol (4) were isolated from an endophytic fungus, Acremonium citrinum SS-g13, harboured in the roots of the Chinese medicinal plant Fructus mori. Their structures were determined by analysing MS, NMR, and ECD data. Compound 1 was evaluated for its cytotoxic effect, antibacterial activity and quorum sensing inhibitory potential.
Assuntos
Acremonium/química , Plantas Medicinais/microbiologia , Pironas/isolamento & purificação , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Citotoxinas/química , Citotoxinas/isolamento & purificação , Citotoxinas/farmacologia , Endófitos/química , Humanos , Estrutura Molecular , Raízes de Plantas/efeitos dos fármacos , Pironas/química , Percepção de Quorum/efeitos dos fármacosRESUMO
The influence of different reaction conditions on the yield of syringaldehyde was studied by using perovskite oxide as the catalyst. The optimal reaction conditions are as follows: 0.60 g of dealkali lignin, 0.60 g of 5 wt % theta ring-loaded LaFe0.2Cu0.8O3 catalyst, 30 mL of 1.0 mol/L NaOH solution, 160 °C reaction temperature, 0.80 MPa O2 pressure, and 2.5 h reaction time. Under these conditions, the highest syringaldehyde yield was 10.00%. The recycling performance of the catalyst was studied. It was found by XRD analysis that the catalyst maintained high catalytic activity after four times of use.